JP2020519610A - 治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造 - Google Patents

治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造 Download PDF

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JP2020519610A
JP2020519610A JP2019561911A JP2019561911A JP2020519610A JP 2020519610 A JP2020519610 A JP 2020519610A JP 2019561911 A JP2019561911 A JP 2019561911A JP 2019561911 A JP2019561911 A JP 2019561911A JP 2020519610 A JP2020519610 A JP 2020519610A
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alkyl
group
och
formula
antibody
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JP2020519610A5 (enExample
JPWO2018206635A5 (enExample
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エルヴェ・ブーシャール
マリー−プリシーレ・ブラン
フィリップ・ユベール
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Sanofi SA
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Sanofi SA
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Publication of JP2020519610A5 publication Critical patent/JP2020519610A5/ja
Publication of JPWO2018206635A5 publication Critical patent/JPWO2018206635A5/ja
Priority to JP2023061810A priority Critical patent/JP2023085475A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15—Depsipeptides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • A61K47/6829—Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Toxicology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2019561911A 2017-05-10 2018-05-09 治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造 Pending JP2020519610A (ja)

Priority Applications (1)

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JP2023061810A JP2023085475A (ja) 2017-05-10 2023-04-06 治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17305531.0 2017-05-10
EP17305531 2017-05-10
PCT/EP2018/061989 WO2018206635A1 (en) 2017-05-10 2018-05-09 Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation

Related Child Applications (1)

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JP2023061810A Division JP2023085475A (ja) 2017-05-10 2023-04-06 治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造

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JP2020519610A true JP2020519610A (ja) 2020-07-02
JP2020519610A5 JP2020519610A5 (enExample) 2021-05-20
JPWO2018206635A5 JPWO2018206635A5 (enExample) 2022-08-12

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JP2023061810A Pending JP2023085475A (ja) 2017-05-10 2023-04-06 治療において有用な、ペプチド性リンカーおよびクリプトフィシンコンジュゲート、ならびにこれらの製造

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US (5) US20180369401A1 (enExample)
EP (1) EP3621658A1 (enExample)
JP (2) JP2020519610A (enExample)
KR (1) KR102722886B1 (enExample)
CN (1) CN110831633A (enExample)
AR (1) AR111781A1 (enExample)
AU (2) AU2018265333C1 (enExample)
BR (1) BR112019023336A2 (enExample)
CA (1) CA3062977A1 (enExample)
CO (1) CO2019012108A2 (enExample)
EA (1) EA201992667A1 (enExample)
EC (1) ECSP19078277A (enExample)
IL (1) IL270507B2 (enExample)
MA (1) MA50764A (enExample)
MX (1) MX2019013421A (enExample)
MY (1) MY204075A (enExample)
PH (1) PH12019550230A1 (enExample)
TN (1) TN2019000303A1 (enExample)
TW (1) TWI778059B (enExample)
UY (1) UY37728A (enExample)
WO (1) WO2018206635A1 (enExample)

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US11951165B2 (en) 2016-12-30 2024-04-09 Vaxcyte, Inc. Conjugated vaccine carrier proteins
KR20190103256A (ko) 2016-12-30 2019-09-04 수트로박스, 인코포레이티드 비자연 아미노산을 갖는 폴리펩타이드-항원 접합체
TN2019000303A1 (en) 2017-05-10 2021-05-07 Sanofi Sa Peptidic linkers and cryptophycin conjugates, useful in therapy, and their preparation
CN111154133B (zh) * 2020-01-03 2022-07-12 万华化学集团股份有限公司 一种环氧树脂发泡剂，环氧树脂组合物及环氧发泡材料的制备方法和用途
CN114053426B (zh) * 2020-07-30 2024-06-18 成都科岭源医药技术有限公司 一种双药链接组装单元及双药靶向接头-药物偶联物
CN115105607B (zh) * 2021-03-22 2024-12-20 成都科岭源医药技术有限公司 一种用于adc的双药-接头的制备方法及其用途
CN118742328A (zh) 2022-02-22 2024-10-01 阿拉里斯生物技术股份公司 包含两个或更多个有效载荷的肽接头
CN115212315A (zh) * 2022-08-03 2022-10-21 联宁（苏州）生物制药有限公司 一种抗体偶联药物中间体及含有其的抗体偶联药物
WO2025082990A1 (en) 2023-10-15 2025-04-24 Araris Biotech Ag Antibody-drug conjugates using two different types of topoisomerase i inhibitors

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US20200093934A1 (en) 2020-03-26
MX2019013421A (es) 2020-02-05
PH12019550230A1 (en) 2020-07-06
US11007275B2 (en) 2021-05-18
US20200054760A1 (en) 2020-02-20
MY204075A (en) 2024-08-06
KR20200005580A (ko) 2020-01-15
CN110831633A (zh) 2020-02-21
IL270507B1 (en) 2023-04-01
UY37728A (es) 2019-01-02
MA50764A (fr) 2020-03-18
IL270507B2 (en) 2023-08-01
AU2018265333A1 (en) 2019-11-28
US11998611B2 (en) 2024-06-04
AU2022204711C1 (en) 2025-04-24
AU2022204711A1 (en) 2022-07-21
WO2018206635A1 (en) 2018-11-15
AU2022204711B9 (en) 2025-01-23
CO2019012108A2 (es) 2020-02-28
EA201992667A1 (ru) 2020-03-10
TN2019000303A1 (en) 2021-05-07
US20250205348A1 (en) 2025-06-26
EP3621658A1 (en) 2020-03-18
IL270507A (enExample) 2019-12-31
ECSP19078277A (es) 2019-11-30
TWI778059B (zh) 2022-09-21
AU2022204711B2 (en) 2024-01-04
AU2018265333C1 (en) 2025-04-24
AU2018265333B2 (en) 2022-07-21
KR102722886B1 (ko) 2024-10-29
CA3062977A1 (en) 2018-11-15
US20180369401A1 (en) 2018-12-27
US20210228726A1 (en) 2021-07-29
AR111781A1 (es) 2019-08-21
TW201907957A (zh) 2019-03-01
JP2023085475A (ja) 2023-06-20
BR112019023336A2 (pt) 2020-06-16

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